| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Rolapitant (formerly SCH-619734; SCH619734; trade name: Varubi) is a selective, CNS penetrant and orally bioactive neurokinin (NK1) receptor antagonist (Ki = 0.66 nM) with antiemetic activity. It has been approved in 2015 for use along with other medications (eg, dexamethasone) to prevent delayed nausea and vomiting associated with cancer chemotherapy. It functions by obstructing the brain's signals that trigger nausea and vomiting.
| Targets |
human NK1 ( Ki = 0.66 ); gerbil NK1 ( Ki = 0.13 ); guinea pig NK1 ( Ki = 0.72 ); monkey NK1 ( Ki = 2.5 ); rabbit NK1 ( Ki = 31.7 ); rat NK1 ( Ki = 78.6 ); mouse NK1 ( Ki = 60.4 )
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| ln Vitro |
Rolapitant has high selectivity over the human NK2 and NK3 subtypes of more than 1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit[1].
1–1000 nM) inhibits the GR-73632 (an NK1 receptor agonist)–induced calcium efflux in a concentration-dependent and competitive manner in CHO cells expressing the human NK1 receptor[1]. |
| ln Vivo |
Rolapitant (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) areduces the foot-tapping response induced by GR-73632 in Mongolian Gerbils[1].
Rolapitant (0.03–1 mg/kg; PO; single dosage; monitored for 72 hours) prevents acute emesis brought on by cisplatin and apomorphine in ferrets[1]. |
| Animal Protocol |
Female Mongolian Gerbils (30-60 g; anesthetized by inhalation of an oxygen:isofluorane mixture after 4 h PO or immediately after IV, then injected with 5 μl of 3 pmol solution of GR-73632 via ICV)
0.03, 0.1, 0.3 and 1 mg/kg for PO, 0.3 and 1 mg/kg for IV PO or IV, single dosage |
| References |
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| Molecular Formula |
C25H26F6N2O2
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| Molecular Weight |
500.49
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| Exact Mass |
500.19
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| Elemental Analysis |
C, 60.00; H, 5.24; F, 22.78; N, 5.60; O, 6.39
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| CAS # |
552292-08-7
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| Related CAS # |
Rolapitant hydrochloride; 858102-79-1; Rolapitant hydrochloride hydrate; 914462-92-3
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| Appearance |
Solid powder
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| SMILES |
C[C@H](C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC[C@]2(CC[C@]3(CCC(=O)N3)CN2)C4=CC=CC=C4
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| InChi Key |
FIVSJYGQAIEMOC-ZGNKEGEESA-N
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| InChi Code |
InChI=1S/C25H26F6N2O2/c1-16(17-11-19(24(26,27)28)13-20(12-17)25(29,30)31)35-15-23(18-5-3-2-4-6-18)10-9-22(14-32-23)8-7-21(34)33-22/h2-6,11-13,16,32H,7-10,14-15H2,1H3,(H,33,34)/t16-,22-,23-/m1/s1
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| Chemical Name |
(5S,8S)-8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,9-diazaspiro[4.5]decan-2-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9980 mL | 9.9902 mL | 19.9804 mL | |
| 5 mM | 0.3996 mL | 1.9980 mL | 3.9961 mL | |
| 10 mM | 0.1998 mL | 0.9990 mL | 1.9980 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00539721 | Completed | Drug: Rolapitant Dose 1 Drug: Rolapitant Dose 2 |
Postoperative Nausea and Vomiting |
Merck Sharp & Dohme LLC | October 2007 | Phase 2 |
| NCT02434861 | Completed | Drug: Rolapitant Drug: Digoxin Drug: Sulfasalazine |
Chemotherapy-induced Nausea and Vomiting |
Tesaro, Inc. | May 2015 | Phase 1 |
| NCT02382666 | Completed | Drug: Rolapitant | Chemotherapy-induced Nausea and Vomiting |
Tesaro, Inc. | January 2015 | Phase 1 |
| NCT01500213 | Completed | Drug: Rolapitant Drug: Granisetron Drug: Placebo |
Chemotherapy-induced Nausea and Vomiting |
UCB Pharma | February 2012 | Phase 3 |
| NCT01500226 | Completed | Drug: Rolapitant Drug: Granisetron |
Chemotherapy-induced Nausea and Vomiting |
Tesaro, Inc. | February 2012 | Phase 3 |
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